1. Protein Tyrosine Kinase/RTK
  2. FGFR
  3. NOTA-cRY9M

NOTA-cRY9M is a reagent targeting FGFR1 with a Kd value of 58 nM, and exhibits subtype selectivity for FGFR2-4. When radiolabeled as [68Ga]Ga-NOTA-cRY9M, it functions as a stabilizer, imaging contrast enhancer, and tumor-targeting agent, and accumulates in FGFR1-positive non-small cell lung cancer xenograft models. NOTA-cRY9M can be used in studies related to non-small cell lung cancer.

For research use only. We do not sell to patients.

Custom Peptide Synthesis

NOTA-cRY9M

NOTA-cRY9M Chemical Structure

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Description

NOTA-cRY9M is a reagent targeting FGFR1 with a Kd value of 58 nM, and exhibits subtype selectivity for FGFR2-4. When radiolabeled as [68Ga]Ga-NOTA-cRY9M, it functions as a stabilizer, imaging contrast enhancer, and tumor-targeting agent, and accumulates in FGFR1-positive non-small cell lung cancer xenograft models. NOTA-cRY9M can be used in studies related to non-small cell lung cancer[1].

IC50 & Target[1]

FGFR1

58 nM (Kd)

In Vitro

68Ga]Ga-NOTA-cRY9M (74 kBq per well; 15-120 min) exhibits time-dependent, FGFR1-specific cellular uptake in Calu-3 and NCI-H520 NSCLC cells, with significantly lower uptake in FGFR1-negative NCI-H2170 cells[1].
[68Ga]Ga-NOTA-cRY9M (74 kBq per well; 10-11-10-2 M unlabeled peptide; 2 h) exhibits high FGFR1-binding affinity in Calu-3 cells, with an IC50 of 62 nM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

68Ga]Ga-NOTA-cRY9M (3.7 MBq; i.v.; single dose) exhibits superior tumor-targeting efficacy in FGFR1-high NSCLC xenografts, achieving a maximum tumor uptake of 3.69 %ID/g and a peak tumor-to-muscle ratio of 5.56[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c nude (male, 4-5 weeks old, 18-21 g)[1]
Dosage: 3.7 MBq
Administration: i.v.; single dose
Result: Achieved peak tumor uptake of 3.69 %ID/g at 10 minutes postinjection, with uptake declining gradually to 3.33 %ID/g by 60 minutes.
Reached a maximum tumor-to-muscle ratio of 5.56 at 60 minutes, with tumor-to-liver and tumor-to-lung ratios reaching approximately 2.3 and 3.3, respectively, at 60 minutes.
Exhibited primarily renal excretion with low hepatic retention.\nAchieved peak tumor uptake of 3.11 %ID/g at 10 minutes postinjection.
Reached a maximum tumor-to-muscle ratio of 4.10 at 60 minutes.
Showed tumor uptake of 2.61 %ID/g in ex vivo biodistribution at 60 minutes.\nAchieved a maximum tumor uptake of 1.20 %ID/g, with a consistently low tumor-to-muscle ratio of 1.42 throughout the 60-minute imaging window.
Showed tumor uptake of 0.91 %ID/g in ex vivo biodistribution at 60 minutes.\nShowed a substantial reduction in [68Ga]Ga-NOTA-cRY9M uptake (1.10 %ID/g) in FGFR1-knockdown Calu-3 xenografts compared to control Calu-3 tumors (3.83 %ID/g), with a corresponding tumor-to-muscle ratio of 2.11 vs. 5.89 in controls.
Molecular Weight

1597.78

Formula

C71H108N26O17

Sequence

Cyclo(Arg-Trp-Arg-{Lys(NOTA)}-Gln-Thr-Arg-His-Tyr)

Sequence Shortening

Cyclo(RWR-{Lys(NOTA)}-QTRHY)

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
NOTA-cRY9M
Cat. No.:
HY-P11852
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